Art. -Nr.: HY-157039

RIPK1-IN-17

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RIPK1-IN-17 is an orally active, selective RIPK1 inhibitor (K_d = 17 nM) and shows no significant inhibition to RIPK3. RIPK1-IN-17 specifically inhibits necroptosis rather than apoptosis by inhibiting RIPK1, RIPK3, and MLKL phosphorylation. RIPK1-IN-17 protects mice from hypothermia and death. RIPK1-IN-17 can be used for the study of necroptosis-related diseases such as inflammatory response syndrome (SIRS).

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Reinheit: 97.09%
CAS. Nr.: 3033385-59-7
Formel: C₂₆H₁₉F₄N₃O₃S
Molecular Weight:529.51

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

RIPK1-IN-17 Chemical Structure

CAS. Nr.: 3033385-59-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

RIPK1

17 nM (Kd)

Alle RIP kinase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HT-29	CC₅₀	>10 μM Compound: 10	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 16 to 24 hrs by CellTiter-Glo Luminescent cell viability assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 16 to 24 hrs by CellTiter-Glo Luminescent cell viability assay	[PMID: 37917221]
HT-29	EC₅₀	0.017 μM Compound: 10	Anti-necroptic activity against human HT-29 cells assessed as inhibition of TSZ (TNFalpha, Smac mimetic and z-VAD-FMK) induced necroptosis pretreated with compound followed by TSZ stimulation for 16 to 18 hrs by CellTiter-Glo Luminescent cell viability as Anti-necroptic activity against human HT-29 cells assessed as inhibition of TSZ (TNFalpha, Smac mimetic and z-VAD-FMK) induced necroptosis pretreated with compound followed by TSZ stimulation for 16 to 18 hrs by CellTiter-Glo Luminescent cell viability as	[PMID: 37917221]

In Vitro

RIPK1-IN-17 (Compound 10), which is formed by directly connecting two moieties using a biphenyl-type linker, exhibits significantly enhanced activity against necroptosis in HT-29 cells (EC₅₀ = 0.017 μM) and demonstrates no significant cytotoxicity at the tested concentrations (CC₅₀ > 10 μM)^[1].
RIPK1-IN-17 displays significantly enhanced RIPK1 inhibitory activity (K_d = 17 nM) and demonstrates no apparent activity toward RIPK3 at a concentration of 5000 nM^[1].
RIPK1-IN-17 (0.015-0.5 μM) provides dose-dependent protection against TNF-α, Cycloheximide (HY-12320), and Z-VAD-FMK (HY-16658B) (TCZ)-induced necroptosis in HT-29 cells^[1].
RIPK1-IN-17 (0.015-0.5 μM) exhibits protective effects against necroptosis induced by Z-VAD-FMK (HY-16658B) at a lower concentration in murine L929 cells^[1].
RIPK1-IN-17 (0.1-1 μM) shows no protection against apoptosis induced by Cycloheximide or Smac mimetic (in HT-29 cells, even at concentrations up to 1 μM^[1].
RIPK1-IN-17 (1 nM-1 μM, 0-6 h) at a concentration of 1 μM over 6 hours exhibits complete inhibition of RIPK1 phosphorylation, and at doses ranging from 1 to 1000 nM for 6 hours, it inhibits the phosphorylation of RIPK1, RIPK3, and MLKL in a dose-dependent manner in HT-29 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

HT-29 cells
Concentration:

1 μM
Incubation Time:

0 h, 2 h, 4 h, 6 h
Result:

Completely inhibited RIPK1 phosphorylation and subsequently reduced downstream phosphorylation of RIPK3 and MLKL.

Western Blot Analysis^[1]

Cell Line:

HT-29 cells
Concentration:

1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time:

6 h
Result:

Dose-dependently inhibited TSZ-induced phosphorylation of RIPK1, RIPK3, and MLKL.

In Vivo

RIPK1-IN-17 (1.25-5 mg/kg, oral gavage, once) effectively protects mice from TNFα-induced SIRS, as demonstrated by preventing hypothermia, improving survival, and reducing the levels of key proinflammatory cytokines (IL-6 and IL-1β)^[1].
RIPK1-IN-17 (100 mg/kg, 200 mg/kg, oral gavage, once) shows good tolerability and safety at doses far above its effective therapeutic dose in mice, without causing acute toxic reactions or organ damage^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male C57BL/6 J mice aged 6-8 weeks injected mTNFα^[1].
Dosage:

1.25 mg/kg, 2.5 mg/kg, 5 mg/kg
Administration:

Oral gavage, once, two hours before injection of mTNFα
Result:

The survival rates of the SIRS mice were indicated as 70, 80, and 100%.
Significantly shielded the SIRS mice from hypothermia and death at the dosages of 1.25, 2.5, or 5 mg/kg.
Significantly reduced the levels of IL-6 and IL-1β in different tissues.
Dose-relatedly decreased the levels of IL-6 in the heart, liver, spleen, lung, kidney, intestine, and brain.
Led to a significant decrease in IL-1β levels in the spleen, lung, and intestine, which are the main organs affected in SIRS models.
Significantly decreased serum levels of IL-1β (three doses) and IL-6 (high dose).

Animal Model:

Male C57BL/6 J mice aged 6-8 weeks^[1].
Dosage:

100 mg/kg, 200 mg/kg
Administration:

Oral gavage, once
Result:

No deaths or weight loss were observed after intragastric administration of the doses. Exhibited normal behavior throughout the 2-week study period.
Hematoxylin-Eosin (HE) staining assays revealed no significant pathological damage to the six vital organs (heart, liver, spleen, lung, kidney, and brain).

Chemical Information

CAS. Nr. 3033385-59-7
Appearance Solid
Molecular Weight 529.51
Formel C₂₆H₁₉F₄N₃O₃S
Color White to off-white
SMILES

O=C(CC1=CC=CC(OC(F)(F)F)=C1)NC2=C(C=CC(C3=CC=C4N=C(SC4=C3)NC(C5CC5)=O)=C2)F
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Fang JJ, et al. Insight from Linker Investigations: Discovery of a Novel Phenylbenzothiazole Necroptosis Inhibitor Targeting Receptor-Interacting Protein Kinase 1 (RIPK1) from a Phenoxybenzothiazole Compound with Dual RIPK1/3 Targeting Activity. J Med Chem. 2023 Nov 2. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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RIPK1-IN-17

Oxygen Sensing Compound Library

Pyroptosis Compound Library

Anti-Obesity Compound Library

Highly Selective Inhibitors Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

NF-κB Signaling Compound Library

Alle RIP kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

RIPK1-IN-17

Oxygen Sensing Compound Library

Pyroptosis Compound Library

Anti-Obesity Compound Library

Highly Selective Inhibitors Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

NF-κB Signaling Compound Library

Alle RIP kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

RIPK1-IN-17 Related Classifications

HY-157039 Related Classifications